BRPI0605934A2 - processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba - Google Patents

processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba

Info

Publication number
BRPI0605934A2
BRPI0605934A2 BRPI0605934-1A BRPI0605934A BRPI0605934A2 BR PI0605934 A2 BRPI0605934 A2 BR PI0605934A2 BR PI0605934 A BRPI0605934 A BR PI0605934A BR PI0605934 A2 BRPI0605934 A2 BR PI0605934A2
Authority
BR
Brazil
Prior art keywords
compound
fluorophenyl
processes
preparing
azetidinone
Prior art date
Application number
BRPI0605934-1A
Other languages
English (en)
Inventor
Vinod Kumar Kansal
Sunhail Ahmad
Bhupendra Tyagi
Nitin Gupta
Nurit Perlman
Original Assignee
Teva Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Teva Pharma filed Critical Teva Pharma
Publication of BRPI0605934A2 publication Critical patent/BRPI0605934A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

PROCESSOS PARA A PREPARAçãO DE (3R,4S)-4-((4-BENZILOXI)FENIL)-1-(4-FLUOROFENIL)-3-((S)-3-(4-F LUOROFENIL)-3-HIDROXIPROPIL)-2-AZETIDINONA, UM INTERMEDIáRIO PARA A SìNTESE DE EZETIMIBA. A invenção abrange (3R,4S)-4-((4-benziloxi)fenil)-1-(4-fluorofenil)-3-(4-fluorofenil)-3-oxopro pil)-2-azetidinona (Composto 2a) tendo uma pureza enanciomérica de pelo menos cerca de 97,5%. A invenção também abrange o Composto 2a tendo uma pureza química de pelo menos 97%. A invenção abrange adicionalmente processos para preparar o Composto 2a a partir do Composto 1 tendo a seguinte fórmula (1) . Composto 1. A invenção abrange também processos para preparar um composto tendo a fórmula (II), a partir de um composto tendo a seguinte fórmula (III), em que R é selecionado no grupo que consiste de: H ou um grupo protetor de hidroxil. A invenção também abrange processos para preparar o Composto 2a, preferivelmente para formar o Composto 2a-Eorma 01. Também inclui processos para preparar ezetimiba a partir do Composto 2a-Forma 01 ou Composto 2a preparado de acordo com a invenção, composições contendo a referida ezetimiba e métodos para reduzir o colesterol usando as referidas composições.
BRPI0605934-1A 2005-09-08 2006-09-08 processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba BRPI0605934A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US71591905P 2005-09-08 2005-09-08
US83243006P 2006-07-20 2006-07-20
PCT/US2006/035060 WO2007030721A2 (en) 2005-09-08 2006-09-08 Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe

Publications (1)

Publication Number Publication Date
BRPI0605934A2 true BRPI0605934A2 (pt) 2009-05-26

Family

ID=37671943

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0605934-1A BRPI0605934A2 (pt) 2005-09-08 2006-09-08 processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba

Country Status (9)

Country Link
US (2) US20070259845A1 (pt)
EP (1) EP1922304A2 (pt)
JP (1) JP2008517951A (pt)
KR (1) KR20070063592A (pt)
BR (1) BRPI0605934A2 (pt)
CA (1) CA2616058A1 (pt)
IL (1) IL186326A0 (pt)
MX (1) MX2007005493A (pt)
WO (1) WO2007030721A2 (pt)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0215579D0 (en) 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
WO2005044256A1 (en) * 2003-10-30 2005-05-19 Merck & Co., Inc. 2-azetidinones as anti-hypercholesterolemic agents
ATE485267T1 (de) 2003-12-23 2010-11-15 Astrazeneca Ab Diphenylazetidinonderivate mit die cholesterinabsorption hemmender wirkung
UY29607A1 (es) 2005-06-20 2007-01-31 Astrazeneca Ab Compuestos quimicos
AR057072A1 (es) 2005-06-22 2007-11-14 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto
SA06270191B1 (ar) 2005-06-22 2010-03-29 استرازينيكا ايه بي مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم
HUP0501164A2 (en) * 2005-12-20 2007-07-30 Richter Gedeon Nyrt New industrial process for the production of ezetimibe
DE602006009845D1 (de) * 2005-12-22 2009-11-26 Medichem Sa Verfahren zur herstellung von zwischenprodukten für die herstellung von ezetimibe
MX2008010235A (es) * 2006-02-16 2008-10-23 Kotobuki Pharmaceutical Co Ltd Metodo para producir alcohol opticamente activo.
MX2008011418A (es) * 2006-03-06 2008-09-22 Teva Pharma Composiciones de ezetimibe.
AR060216A1 (es) * 2006-03-29 2008-06-04 Medichem Sa Procesos para preparar ezetimibe y compuestos intermediarios utiles para su preparacion
TW200811098A (en) 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
WO2008032338A2 (en) * 2006-09-11 2008-03-20 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe and its intermediates
EP1953140A1 (en) * 2007-01-24 2008-08-06 Krka Process for the preparation of ezetimibe and derivatives thereof
EA017349B1 (ru) * 2007-01-24 2012-11-30 Крка Способ получения эзетимиба и его производных
WO2008151324A1 (en) * 2007-06-07 2008-12-11 Teva Pharmaceutical Industries Ltd. Reduction processes for the preparation of ezetimibe
US20090047716A1 (en) * 2007-06-07 2009-02-19 Nurit Perlman Reduction processes for the preparation of ezetimibe
US20090093627A1 (en) * 2007-08-30 2009-04-09 Lorand Szabo Process for preparing intermediates of ezetimibe by microbial reduction
US8013189B2 (en) * 2007-09-21 2011-09-06 Basf Se Accelerated amide and ester reductions with amine boranes and additives
CZ2007843A3 (cs) * 2007-11-30 2009-06-10 Zentiva, A. S. Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu a jeho meziprodukty
CZ2008317A3 (cs) * 2008-05-21 2009-12-02 Zentiva, A. S. Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu
EP2149547A1 (en) * 2008-07-30 2010-02-03 LEK Pharmaceuticals D.D. Process for the synthesis of ezetimibe and intermediates useful therefor
AR074752A1 (es) * 2008-12-17 2011-02-09 Hanmi Pharm Ind Co Ltd Metodo para preparar ezetimiba e intermediarios usados en la misma
WO2010113175A2 (en) 2009-04-01 2010-10-07 Matrix Laboratories Ltd Enzymatic process for the preparation of (s)-5-(4-fluoro-phenyl)-5-hydroxy- 1morpholin-4-yl-pentan-1-one, an intermediate of ezetimibe and further conversion to ezetimibe
HUE026367T2 (en) 2010-05-04 2016-06-28 Codexis Inc Biocatalysts for ezetimibe synthesis
WO2014019166A1 (zh) * 2012-08-01 2014-02-06 上海威智医药科技有限公司 高活性硼烷类化合物的工业化生产方法
WO2015039675A1 (en) 2013-09-23 2015-03-26 Pharmathen S.A. Novel process for the preparation of ezetimibe intermediates
JP6795974B2 (ja) * 2014-03-06 2020-12-02 日産化学株式会社 光学活性アゼチジノン化合物の製造方法
US11126809B2 (en) 2019-11-08 2021-09-21 Zebra Technologies Corporation Bioptic barcode readers
CN114621126B (zh) * 2020-12-12 2023-07-25 重庆圣华曦药业股份有限公司 一种改进的依折麦布的制备方法
EP4373800A4 (en) * 2021-07-23 2025-10-15 Blackstone Therapeutics Llc PROCESS FOR THE PREPARATION OF HEXAHYDROCANNABINOL
US20250206692A1 (en) * 2022-03-14 2025-06-26 Colorado Chromatography, Llc Hydrogenation of cannabigerol and cannabichromene
CN115453004B (zh) * 2022-10-08 2023-10-13 南京科默生物医药有限公司 一种依折麦布阿托伐他汀钙片中有关物质的检测方法

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2525125B2 (ja) * 1991-07-23 1996-08-14 シェリング・コーポレーション 血清コレステロ―ル低下薬として有用な置換β−ラクタム化合物およびそれらの製法
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
WO1997016424A1 (en) * 1995-11-02 1997-05-09 Schering Corporation Process for preparing 1-(4-fluorophenyl)-3(r)-(3(s)-hydroxy-3-([phenyl or 4-fluorophenyl])-propyl)-4(s)-(4-hydroxyphenyl)-2-azetidinone
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US5739321A (en) * 1996-05-31 1998-04-14 Schering Corporation 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
US6982251B2 (en) * 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
CA2439920A1 (en) * 2001-03-08 2002-09-19 Merck & Co., Inc. Antihypertensive agent and cholesterol absorption inhibitor combination therapy
DK1373230T3 (da) * 2001-03-28 2005-11-07 Schering Corp Enantiselektiv syntese af azetidinon mellemprodukter
US20030119808A1 (en) * 2001-09-21 2003-06-26 Schering Corporation Methods of treating or preventing cardiovascular conditions while preventing or minimizing muscular degeneration side effects
JP4589919B2 (ja) * 2003-03-07 2010-12-01 シェーリング コーポレイション 高コレステロール血症の処置のための、置換アゼチジノン化合物、これらの処方物および使用
AU2003282384A1 (en) * 2003-11-24 2005-06-08 Hetero Drugs Limited A novel process for ezetimibe intermediate
US20050171080A1 (en) * 2003-12-23 2005-08-04 Dr. Reddy's Laboratories, Inc. Polymorphs of ezetimibe and process for preparation thereof
US20060160785A1 (en) * 2004-12-03 2006-07-20 Judith Aronhime Ezetimibe polymorphs
CN102633730A (zh) * 2004-12-03 2012-08-15 先灵公司 作为cb1拮抗剂的取代哌嗪
EP1831162B1 (en) * 2004-12-20 2012-10-31 Merck Sharp & Dohme Corp. Process for the synthesis of azetidinones
US20060234996A1 (en) * 2005-04-14 2006-10-19 Itai Adin Novel crystalline form of ezetimibe and processes for the preparation thereof
WO2006137080A1 (en) 2005-06-22 2006-12-28 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe
US20070049748A1 (en) * 2005-08-26 2007-03-01 Uppala Venkata Bhaskara R Preparation of ezetimibe
DE602006009845D1 (de) * 2005-12-22 2009-11-26 Medichem Sa Verfahren zur herstellung von zwischenprodukten für die herstellung von ezetimibe
MX2008010235A (es) * 2006-02-16 2008-10-23 Kotobuki Pharmaceutical Co Ltd Metodo para producir alcohol opticamente activo.
WO2007108007A1 (en) * 2006-03-23 2007-09-27 Unichem Laboratories Limited A process for the preparation of ezetimibe via a novel intermediate
US20080032964A1 (en) * 2006-04-10 2008-02-07 Kansal Vinod K Process for the synthesis of azetidinone
WO2008027081A1 (en) * 2006-08-29 2008-03-06 Teva Pharmaceutical Industries Ltd. Processes for the purification of (3r,4s)-4-(4-hydroxy-protected-phenyl)-1-(4-fluorophenyl)-3-(4-fluorophenyl)-3-oxopropyl] azetidin-2-one
US20090047716A1 (en) * 2007-06-07 2009-02-19 Nurit Perlman Reduction processes for the preparation of ezetimibe

Also Published As

Publication number Publication date
EP1922304A2 (en) 2008-05-21
MX2007005493A (es) 2007-09-11
WO2007030721A9 (en) 2008-04-24
US20070259845A1 (en) 2007-11-08
WO2007030721A2 (en) 2007-03-15
WO2007030721A3 (en) 2007-05-31
JP2008517951A (ja) 2008-05-29
IL186326A0 (en) 2008-01-20
US20100010212A1 (en) 2010-01-14
CA2616058A1 (en) 2007-03-15
KR20070063592A (ko) 2007-06-19

Similar Documents

Publication Publication Date Title
BRPI0605934A2 (pt) processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba
MXPA04003007A (es) Compuestos azabiciclico sustituidos condensados con heteroarilo para el tratamiento de enfermedades.
MXPA04000677A (es) Tienopirimidindionas y su uso en modulacion de enfermedades autoinmunes.
NO20080416L (no) Forbedrede prosesser for fremstilling av Ezetimibe
NO20063501L (no) Kinolinintermediater av reseptor-Tyrosin-Kinase-inhibitorer og deres syntese
EA200300970A1 (ru) Энантиоселективный синтез промежуточных соединений для получения азетидинонов
MXPA04004464A (es) Compuestos de heteroarilo sustituido con azabiciclo para el tratamiento de enfermedades.
BRPI0507005A (pt) compostos, composições farmacêuticas, uso de um composto, e, método de preparo de uma composição farmacêutica
NO20055688L (no) Organiske forbindelser
WO2007119106A3 (en) Processes for preparing intermediate compounds useful for the preparation of ezetimibe
MA32104B1 (fr) Dérivés d'oxime en tant qu'inhibiteurs de hsp90
BRPI0519496A2 (pt) processo para preparar um composto ou uma composiÇço, e, composiÇço
WO2008032338A3 (en) Improved process for the preparation of ezetimibe and its intermediates
TW200510317A (en) Caspase inhibitors and uses thereof
TNSN04250A1 (en) Diphenyl azetidinones substituted by acidic groups, method for their production, medicaments containing said compounds and use thereof.
NO20082747L (no) Arylisoksazol-4-yl-imidazolderivater
IL183373A0 (en) 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives, pharmaceutical compositions containing the same and methods for the preparation thereof
BRPI0417157A (pt) composto, composição farmacêutica, e, uso de um composto ou de uma composição farmacêutica
MXPA05013772A (es) 4-(aminometil)-piperidin benzamidas como antagonistas de 5ht4.
EA200700166A1 (ru) 4-замещённые производные хинолина, способ получения и промежуточные вещества для их приготовления и содержащие их фармацевтические композиции
WO2005085236A3 (en) Caspase inhibitors and uses thereof
ATE454383T1 (de) Neue verbindungen, deren verwendung und herstellung
ATE372332T1 (de) Verfahren zur herstellung von zwischenverbindungen in der herstellung von discodermolid und discodermolid-analoga
WO2006112742A3 (en) PROCESS FOR PREPARATION OF 13,14-DIHYDRO-PGF2α DERIVATIVES
WO2006066044A3 (en) Processes for producing 4-aminoquinazolines

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 4A E 5A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012.